COMPOSITAE (ASTERACEAE) Carthamus tinctorius  L.

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[1] EFFECTS OF HYDROXYSAFFLOR YELLOW A ON THE ACTIVITY AND MRNA EXPRESSION OF FOUR CYP ISOZYMES IN RATS.
REN-AI XU,ZHI-SHENG XU , REN-SHAN GE
J ETHNOPHARMACOL 2014 Vol.151(),1141-46  $50677 [Full]

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; After pretreatment with HSYA, the t1/2, Tmax, C max, AUC (0- infinity) and MRT (0-infinity) of phenacetin in LLG were increased significantly by 36.2%, 33.3%, 32.9%, 94.6% and 74.9% (P<0.05) compared to those of BCG, CL of phenacetin in LLG was decreased significantly by 46.3% (P<0.05).
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; The t1/2, Tmax, Cmax, AUC (0- infinity) and MRT (0-infinity) of phenacetin in HLG were increased significantly by 63.8%, 52.6%, 82.6%, 193.5% and 78.7% (P<0.05) compared to those of BCG, CL of phenacetin in HLG was decreased significantly by 46.5% (P<0.05).
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg/day
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg/day
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg/day
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Positive
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg/day
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Positive
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.


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